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Bioorg Med Chem Lett. 2007 Jan 15;17(2):471-5. Epub 2006 Oct 12.

Synthesis and biological evaluation of novel T-type calcium channel blockers.

Author information

1
Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, 1 Hoegi-Dong, Seoul 130-701, Republic of Korea.

Abstract

3,4-Dihydroquinazoline analogues substituted by N-methyl-N-(5-pyrrolidinopentyl)amine at the 2-position were synthesized and their blocking effects were evaluated for T- and N-type calcium channels. Compound 11b (KYS05080), compared to mibefradil (IC50=1.34+/-0.49 microM), was about 5-fold potent (IC50=0.26+/-0.01 microM) for T-type calcium channel (alpha1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil).

PMID:
17064894
DOI:
10.1016/j.bmcl.2006.10.024
[Indexed for MEDLINE]

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